JNJ-26481585

JNJ-26481585 (Quisinostat) is an oral histone deacetylase (HDAC) inhibitor with IC50 values of 0.11 nM, 0.33 nM, 0.64 nM, 0.46 nM and 0.37 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11, respectively. JNJ-26481585 fully inhibited the growth of C170HM2 colorectal liver metastases, whereas again 5-fluorouracil/Leucovorin showed modest activity. JNJ-26481585 exhibits broad spectrum antiproliferative activity in solid and hematologic cancer cell lines, such as all lung, breast, colon, prostate, brain, and ovarian tumor cell lines, with IC50 ranging from 3.1-246 nM, which is more potent than vorinostat, R306465, panobinostat, CRA-24781, or mocetinostat in various human cancer cell lines tested. Once daily oral administration of JNJ-26481585 induced continuous histone H3 acetylation. JNJ-26481585 is currently in a phase II clinical trial for the treatment of previously treated cutaneous T-cell lymphoma.